Primaquine
Indications
Primaquine is used for:
Malaria
Adult Dose
Oral
Prevention of relapse of P. vivax malaria
30 mg PO qDay for 14 days
Uncomplicated P. vivax and P. ovale malaria
30 mg PO qDay for 14 days with chloroquine or hydroxychloroquine
Alternatively, for mild G6PD deficiency or as alternative to daily regimen: 45 mg PO qDay for 8 weeks (only to be used after consultation with an infectious disease/tropical medicine expert
Chemoprophylaxis
P. vivax and P. ovale maleria: 30 mg PO qDay for 14 days after departure from malaria-endemic area
Child Dose
Oral
Uncomplicated P. vivax and P. ovale malaria
0.5 mg/kg (30 mg/day maximum) qDay for 14 days with chloroquine or hydroxychloroquine
Chemoprophylaxis
0.5 mg/kg PO qDay (30 mg/day maximum); start 1-2 days prior to travel and continue for 7 days after departure from malaria endemic area
Renal Dose
Administration
Should be taken with food. Take w/ meals to avoid GI discomfort.
Contra Indications
Hypersensitivity. Childn <1 yr. Acute flare-ups of systemic diseases (RA, SLE) having tendency for agranulocytopaenia, Pregnancy and lactation.
Precautions
G6PD deficiency; pregnancy; NADH methaemoglobin reductase deficient patients. Monitor Hb levels and blood counts routinely. Patients with systemic diseases that have an increased risk of granulocytopenia. Withdraw treatment if signs of haemolysis or methaemogloinaemia occur.
Pregnancy-Lactation
Pregnancy
Contraindicated in pregnant women; even if a pregnant woman is G6PD normal, the fetus may not be; safe usage in pregnancy not established; use during pregnancy should be avoided except when in judgment of the physician benefit outweighs possible hazard
Sexually-active females of reproductive potential should have a pregnancy test prior to starting primaquine
Contraception
Advise females of child bearing potential to use effective contraception (methods that result in less than 1% pregnancy rates) when receiving therapy and after stopping treatment until completion of an ongoing ovulatory cycle (eg, up to next menses)
Advise treated males whose partners may become pregnant, to use a condom while on treatment and for 3 months after stopping treatment
Lactation
CDC recommends do not use in nursing women unless breast-fed infant has been determined not to have G6PD deficiency
Interactions
Primaquine may inhibit metabolism of chloroquine. Avoid ethanol.
Potentially Fatal: Mepacrine may potentiate toxicity of primaquine. Potentially haemolytic drugs eg, sulphonamides, nitrofurans and bone marrow suppressants eg, methotrexate, phenylbutazone, chloramphenicol should not be co-admin with primaquine.
Adverse Effects
Side effects of Primaquine :
>10%
Abdominal pain, Hemolytic anemia in G6PD deficiency, Nausea, Vomiting
<1-10%
Methemoglobinemia in NADH-methemoglobin reductase-deficient individuals
<1%
Agranulocytosis, Arrhythmias, Headache, Interference with visual accommodation, Leukopenia, Leukocytosis, Rash, Dizziness, Pruritus
Potentially Fatal: Haemolytic anaemia (G6PD deficient), thrombocytopaenia, leucopaenia, AV block.
Mechanism of Action
Primaquine is an 8-aminoquinoline antimalarial which eliminates the exoerythrocytic forms of malarial parasite P.vivax, P. falciparum by disrupting mitochondria and binding to DNA. By this action primaquine achieves radical cure of vivax malaria. It is also active against gametocytes of P.falciparum.